Method for preparing a hypericum extract in neem oil and a substance so obtained

ABSTRACT

A method for making a  Hypericum perforatum  extract in Neem oil, provides of:
         combining an amount of  Hypericum  flowers and/or capsules with a quantity of Neem oil;   introducing into a reactor the mixture made of the amounts of  Hypericum  flowers and/or capsules and of Neem oil;   maintaining the mixture vacuum, under agitation for a predefined time and temperature. A composition includes Neem oil and  Hypericum  flowers and/or capsules. Such composition includes moreover a solvent or a mixture of solvents.

TECHNICAL FIELD

This invention relates to medical-surgical devices, in particular refersto a method for the preparation of a Hypericum perforatum extract(Hypericum) in Neem oil and to a substance so obtained.

BACKGROUND ART

It is known that the oleolito or the hypericum perforatum extract hasanti-inflammatory effect, antiseptic and cicatrizing in the externalwounds, ulcers and burns.

It is furthermore known that the Neem oil has cicatrizing, biocide, antiinflammatory, myasis insect repellent and not proprieties.

For example it is known in WO 2006/013607 that the oil mixture of Neemand the oily extract of Hypericum perforatum add the bioactivecharacteristics verified in the single components of the mixture.

Said diluting effect precludes to think equivalent the biologic andbiocide properties, of single obtainable compositive mixtures, becausethe biologic property is molecular, depends on the structure anddepending on dose.

In such document WO 2006/013607, for indicated preparation modality, thehypericum oleolito cannot certainly satisfy the reproducibilitycriterion of the obtained oleolito results, considering the loss of theprocess conditions (temperature, time, lighting degree, agitation,drugs/oil ratio), to satisfy the criterion of a minimum reproducibilityof the oleolito molecular composition.

Moreover in the preparation so obtained already at 16° C. developsturbidity because of hydrocarbons, fat acids, etc. precipitation, somodifying the spreading and the use easiness of the preparation. Thisfact decreases the potentiality in the space-time, in relation to theclimate.

Moreover the spagyric maceration used in the extraction processaccording to document WO2006/013607 is subjected to climatic factor(light, temperature) variability and is subjected to process variabletimes.

DISCLOSURE OF THE INVENTION

Object of this invention is to propose an industrial extraction methodof the bioactive substances of Hypericum perforatum flowers andinfructescences (capsules) using as extracting solution of the Neem oilwithout using other oil for the maceration.

Further object is to increase the extraction method for example by usinga solvent.

An additional aim is to obtain Hypericum extracts directly in Neem oilconcentrates and with greater applicability range in function of thetemperature.

An additional aim is furthermore to offer a method highly easy andeconomically advantageous.

BEST MODE OF CARRYING OUT THE INVENTION

The method object of the present invention consists in putting thefresh, frozen, dried, lyophilized Hypericum flowers, and theinfructescences (capsules), or their mixtures into a reactor, consistingof a steel container, equipped with central rotatory axis carrying,inserted on the axis, agitation blades, that can to be rotate withvariable speed. The container carries an air-tight glass cover permeableto the radiations in the visible spectrum field.

The container is heated at vacuum state with depression not lower than0.04 atmospheres.

The ratio value of solvent solution weight / flowers or capsules weightis between 3 and 1 and between 15 and 1 depending on the decreasingwater content of flowers or capsules or the their mixtures. Afterflowers and/or capsule introduction, there is put the solvent chosenbetween:

-   -   a) Neem oil as which;    -   b) mixtures including Neem oil and a solvent or solvents        mixtures, such as benzyl alcohol, ethanol, phenylethyl alcohol,        alphaphenylethyl alcohol, ethyl alcohol, isopropyl alcohol,        octyl alcohol; glycols as glycerin, propylene glycol,        polyethylene glycol; esters as ethyl acetate, octyl acetate,        ethyl lactate, isopropyl acetate, isopropyl myristate, isopropyl        palmitate, ethyl caprylate, ethylphenylacetate, ethyl oleate,        ethyl linoleate, ethyl laurate, triethylcitrate, phenylethyl        acetate; triglycerides as: triolein, trilinolein, tributyrin,        triacetin, tricaprylin, tricaproin, tricaprin, paraffin oils,        silicones, in ratio Neem oil-solvents between 1:2 and 1:0.01.

The listed extraction solvents at items a, b, alone or added withcomponents such as silicones, paraffin oils, esters, triglycerideliquids at 4° C., can unfavorable precipitation phenomena in the topiccomposition during the preservation, widening the applicability rangeuntil temperatures close to 0° C. or lower.

Therefore the vacuum is obtained, the heating of mass of the extractionsolvent and biomass at temperatures ranging between 16° C. and 100° C.is activated and the helicoidal blades shaft is put into rotation.

The irradiation is activated and it is maintained the contact betweenextractant solution and biomass for periods from 1 hour until 400 hours.

When the extraction time is elapsed, the maceration liquid is sent,interposing one or more filters, into dark glass amber colored containerand therein the maceration product is preserved avoiding the contactwith the air oxygen. The extraction kinetics is overseen monitoring, bymeans of HPLC chromatography, the two molecules of marker hypericine andderivatives with 585 nanometers and the hyperphorine and derivativeswith 278 nanometers.

With this method is obtained a composition as anti-inflammatorymedicine, antiseptic and cicatrizing, for example in the treatment ofoutside wounds, ulcers, sores and burns, further acting as repellent formyasis and not insects.

Further features will greatly result from the description of somepractical realization preferred examples of the preparation method ofthe extract according to the invention, examples given hereinafter asindicative and not limitative.

EXAMPLE 1

There are introduced in the reactor 300 grams of Hypericum flowers orHypericum perforatum capsules dried, or frozen or lyophilized, etc. andvacuum is obtained after hermetic sealing of the glass cover of thereactor.

Therefore 4 kg of clear Neem oil are introduced, and when completed thesolvent feeding, the multiple-blade agitator starts up, the temperatureis grown to 50° C. and there is radiation.

After 220 hour the mixing shaft is stopped, and simultaneous is blockedthe heating and the radiation and the extract is transferred into anamber colored glass container.

One or two filtering cartridges for eliminating the suspension materialare inserted in the adducing pipe of the extract. The Hypericum extractin Neem oil is preserved at dark at 20° C.±1.

The extract yield was 2.85 kg equal to 71.25% of the introduced Neemoil.

EXAMPLE 2

300 grams of lyophilized Hypericum flowers (about 2 liters of volume) ofwhich 60% are infructescence are introduced into the reactor and 3.5 kgof extractant solution are added, consisting of Neem oil 41%(weight/weight), 26% of ethyl acetate, 16% of benzyl alcohol, 16% ofethanol at 96%.

The vacuum is obtained, it is programmed the heating to 35° C. and themixing speed is adjusted by fixing the rotation speed of the shaftsupporting the blades, by radiating with white light lamps, for a totalextraction time of 180 hours.

After such period, agitation and irradiation are stopped and the extractis transferred into amber colored glass container.

The recovered extract weight was of 2.8 kg equal to a yield of 80.3% ofthe extractant mixture.

EXAMPLE 3

800 grams of Hypericum capsules or fresh Hypericum flowers are placedinto reactor, both 3.8 kg of extractant solution of the following percent composition: 50% of Neem oil, 15% of alcohol phenyl ethylic, 20% ofpropyl acetate, 10% of ethanol at 96°, 2% of isopropyl palmitate, 3% ofparaffin oil with freezing point at −20° C. and the vacuum is obtained.

The heating is fixed to 65° C., the agitator is activated and, givingthe irradiation, the extraction is continued for 120 hours.

The agitation and the irradiation are stopped and the trial continuesaccording to example 1 by transferring into dark glass container 2.3 kgof extract equal to a yield of 71.8%.

An advantage is to increase the extraction method for example by using asolvent.

An additional advantage is to obtain Hypericum extract in Neem oilconcentrates.

1. A method for preparing a Hypericum perforatum extract in Neem oilcomprising: combining an amount of Hypericum flowers and/or encapsulatedHypericum flowers with a quantity of an extraction solvent being Neemoil present in a weight ratio ranging between 1:3 and 1:15 to provide amixture; introducing the mixture into a reactor; and maintaining themixture under vacuum and agitating for a predefined time ranging betweenone hour and 400 hours and at a temperature ranging between 16° C. and100° C. to produce a macerated product which contains the Hypericumperforatum extract dissolved in the Neem oil.
 2. The method according toclaim 1 further comprising irradiating the mixture with light having avisible spectrum.
 3. The method according to claim 1 wherein theHypericum flowers are fresh, frozen, lyophilized or dried Hypericumflowers.
 4. The method according to claim 1 wherein the vacuum has adepression not lower than 0.04 atmospheres.
 5. The method according toclaim 1 wherein the agitation is variable between 2 and 30 rotations perhour.
 6. The method according to claim 1 wherein the Neem oil isprovided in combination with a solvent or a solvent mixture.
 7. Themethod according to claim 6 wherein the Neem oil comprises at least 33%by weight of the combination with the solvent or mixture of solvents. 8.The method according to claim 6 wherein the solvent is selected from thegroup consisting of alcohols, glycols, esters, triglycerides, paraffinoils, silicones or combinations thereof.
 9. The method according toclaim 6 wherein the solvent is selected from the group consisting ofbenzyl alcohol, ethanol, phenylethyl alcohol, alphaphenylethyl alcohol,ethyl alcohol, isopropyl alcohol, octyl alcohol, glycerin, propyleneglycol, polyethylene glycol, ethyl acetate, octyl acetate, ethyllactate, isopropyl acetate, isopropyl myristate, isopropyl palmitate,ethyl caprylate, ethylphenylacetate, ethyl oleate, ethyl linoleate,ethyl laurate, triethylcitrate, phenylethyl acetate, triolein,trilinolein, tributyrin, triacetin, tricaprylin, tricaproin, tricaprinor combinations thereof.
 10. The method according to claim 1 furthercomprising transferring the extract, after an extraction time haselapsed, into a dark amber colored glass container.
 11. The methodaccording to claim 10 further comprising filtering the extract duringthe transferring to remove suspension material.
 12. The method accordingto claim 1 further comprising preserving the extract by avoiding contactwith oxygen in the air.
 13. A composition comprising a Hypericumperforatum extract in Neem oil obtained by the method of claim
 1. 14.The composition according to claim 13 characterized in that thecomposition is usable as a liquid lotion at a temperature at least aslow as 0° C.
 15. The composition according to claim 13 wherein theextract is obtained from Hypericum flowers or encapsulated Hypericumflowers which are fresh or frozen or lyophilized or triturated beforethe maceration.